The use of marijuana for medicinal and recreational purposes is on the rise among the general population. Along with the rise of use, state laws are now changing to reflect the evolving attitude of the American public. As of early 2016, five jurisdictions have legalized the recreational use of marijuana—Washington, Colorado, Oregon, Alaska, and Washington, D.C. Many more states now allow the medicinal use of marijuana—Alaska, Arizona, California, Colorado, Connecticut, Washington, D.C., Delaware, Hawaii, Illinois, Maine, Maryland, Massachusetts, Michigan, Minnesota, Montana, Nevada, New Hampshire, New Jersey, New Mexico, New York, Oregon, Rhode Island, Vermont, and Washington.
The least contentious use of marijuana is for medicinal purposes. Marijuana has been recognized as an effective treatment for many medical conditions, including but not limited to cancer, anorexia, AIDS, chronic pain, cachexia, persistent muscle spasms, multiple sclerosis, seizures, epilepsy, severe nausea, glaucoma, arthritis, migraine, and any other chronic or persistent medical symptom that substantially limits the ability of the person to conduct one or more major life activities (as defined by the Americans with Disabilities Act of 1990) or, if not alleviated, may cause serious harm to the patient's safety or physical or mental health. The recognized conditions vary by state. However, most jurisdictions permit the use of marijuana for pain management.
There are over 480 natural components found in Cannabis, which include delta-9-tetrahydrocannabinol (commonly referred to as THC) and cannabinoids. Cannabidiol (CBD), cannabinol (CBN), cannabadivarin (THCU), cannabigerol (CBG), cannabichromene (CBC), cannabicyclol (CBL), cannabitriol (CBT), and cannabiscoin (CBE) are some of the many cannabinoids found in the Cannabis plant. Each cannabinoid is structurally similar but differentiated by its interaction with the user's central nervous system receptors. THC is the most well-known component found in marijuana. Many of these components have been studied for its physiological impact on the human body and thus potential use for medical purposes.
The use of tetrahydrocannabinol (THC) and cannabichromene (CBC) in the management of pain has been well documented. THC is a chemical which binds to the specific receptor site; cannabinoid receptor CB1 and CB2. While it is not completely known how THC and CBC alleviate pain, many studies have hypothesized multi-level, non-competitive direct and indirect interaction of the cannabinoid and opioid receptor systems.
Enkephalin is one of three well-defined endogenous opioid peptides found in the body, the other two being endorphins and dynorphins. These substances are known to have potent painkilling properties. Endogenous opioid peptides act as neuromodulators that modify the actions of other neurotransmitters in the central nervous system. The inventor recognizes enkephalin's role in regulating nociception, the ability for the body to interpret harmful stimuli. Enkephalins are internally propagated and bind to the body's opioid receptors.
The opioid receptors, μ-opioid receptors (MOR) and δ-opioid receptors (DOR), contain enkephalins as its binding site protein. The opioid receptors discussed herein are recognized for their analgesic potential and mood modulating roles. It is further recognized that the DOR modulates the nociception of chronic pain whereas the MOR modulates acute pain. Enkephalins are the endogenous ligands which bind to the mentioned opiate receptors described herein. The inventor recognizes that the two forms of enkephalins (Met-enkephalin and Leu-enkephalin) contain the amino acids, Methionine (Met) and Leucine (Leu).
In addition to THC and its interaction with the opioid receptor system, phenylalanine is recognized as an analgesic. Phenylalanine's role as an analgesic is best postulated by its blockage of enkephalin degradation. Phenylalanine has demonstrated to produce naloxone reversible analgesia and consequently increase the analgesic properties of enkephalins. Phenylalanine is the primary precursor for dopamine. The role of dopaminergic neurotransmission is recognized as a natural analgesic within the supraspinal regions and the role of dopamines descending inhibition of pain. Decreased levels of dopamine are probable for increased pain signaling in many animal conditions.
Serine's role participates in the phosphorylation of serine containing analogs and has been recognized to potentiate the blood brain barrier permeability and CNS bioavailability of peptides. This process assists in the biochemical delivery platform of the composition.
Glutamine is one of the few amino acids capable of penetrating the blood brain barrier. Glutamine biosynthesizes glutamate and hence has a two-fold purpose in the composition. It serves in the biosynthesis of γ-aminobutyric acid. Increasing the blood brain barrier penetrating mechanism presents a higher efficacy potential for increased rates of GABA, THC and CBC within the RAIC.
GABA (γ-aminobutyric acid) plays a chief role in reducing neuronal excitability in the nervous system. It is synthesized from glutamate via GAD reaction. It has been demonstrated that the cerebral cortex partakes in the role of regulating pain. When GABA levels are increased in the small region of the cerebral cortex and the rostral angular insular cortex (RAIC), the animal(s) displayed increased and consistent analgesia. This suggests that GABA may function in part to enhance the inhibition of the neurons which illicit pain. By utilizing Glutamine/Glutamate in conjunction with GABA, the potentiating effect on the RAIC is heightened.
The inventor has recognized that the reduction of pain may be enhanced in animals by utilizing the composition which contains the amino acid Phenylalanine, Serine, Glutamine, GABA, and optionally THC, in an ingestible form, and optionally other enumerated components. The organizational blueprint of the claimed composition is designed to biochemically synergize each individual component to elicit a higher rate of efficacy of the enkephalins.